ORAL

CONTRACEPTIVES
Estrogen and Progestin
 INTRODUCTION
• Hormonal preparations used for reversible
suppression of fertility

• Rock and Pincus(1955) announced the

successful use of an oral progestin for
contraception

• As Soon discovered that addition of a small

quantity of an estrogen enhanced their
efficacy
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 INTRODUCTION
• With Oral contraceptives(OCs) fertility can be
suppressed at will, for as long as desired, with
almost 100% confidence & complete return of
fertility on discontinuation

• The efficacy, convenience, low cost and overall

safety of OCs has allowed women to decide if and
when they will become pregnant and to help in
family planning.

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OVULATION

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 USES OF ORAL
CONTRACEPTIVES
• Primary Use
– Prevent pregnancy

• Secondary Uses
– Heavy or irregular menstruation
– Endometriosis
– Polycystic ovary syndrome
– Dysfunctional uterine bleeding

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 COMBINED MODE OF ACTION
OF ESTROGEN AND PROGESTIN
– Prevents ovulation
– Thickens mucous in cervix
– Thins endometrium

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 TYPES OF ORAL
CONTRACEPTIVE PILLS(OCPs)
• Combined pill
• It contain estrogen and a progestin

Progestin Estrogen Trade name

Norgestrel Ethinyl estradiol OVRAL-G
(0.5 mg) (50 mcg)
Levonorgestrel Ethinyl estradiol OVRAL
(0.25 mg) (50 mcg)
Levonorgestrel Ethinyl estradiol OVRAL-L
(0.15 mg) (30 mcg)

Desogestrel Ethinyl estradiol NOVELON

(0.15 mg) (30 mcg)

Desogestrel Ethinyl estradiol FEMILON

(0.15 mg) (20 mcg) 7
 CONTI. . .
• Estrogen and progestins synergise to inhibit ovulation
• The progestin ensures prompt bleeding at the end of the
cycle and blocks the risk of developing endometrial
carcinoma due to estrogen
• One tablet is taken daily for 27 days, starting on the
5th day of menstruation
• The next course is started after a gap of 7 days in which
bleeding occurs

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 PHASED REGIMENS
• Reduction in total steroid dose without compromising
efficacy
• These are biphasic or triphasic
• The estrogen dose is kept constant (or varied slightly
between 30-40 mcg), while the amount of progestin is
low in the first phase and progressively higher in the
second and third phases.
• Phasic pills are particularly recommended for women
over 35 years of age or when other risk factors are
present
Progestin Estrogen Trade name

Levonorgestrel Ethinyl estradiol TRIQUILAR (6 + 5

(50-75-125 mcg) (30-40-30 mcg) + 10 tablets)
Norethindrone Ethinyl estradiol ORTHONOVUM
(0.5-0.75-1.0 mg) (35-35-35 mcg) (7 + 7 + 7 tabs) 9
 Minipill
• It has been devised to eliminate the estrogen, because
many of the long-term risks have been ascribed to this
component
• A low-dose progestin only pill is taken daily continuously
without any gap
• The menstrual cycle tends to become irregular and
ovulation occurs in 20-30% women
• The efficacy is lower (96-98%) compared to 98-99.9%
with combined pill

Progestin Estrogen Trade name

Norethindrone Nil MICRONOR
(0.35 mg)
Norgestrel Nil OVRETTE 10
(75 mcg)
POSTCOITAL (EMERGENCY)
CONTRACEPTION
• Three Regimens are available :-
• (a) Levonorgestrel 0.5 mg + ethinylestradiol 0.1 mg
taken as early as possible but within 72 hours of
unprotected intercourse & reprated after 12 hours
• (b) Levonorgestrel alone (0.75 mg) taken twice with 12
hour gap within 72 hours of intercourse
• (c) Mifepristone 600 mg single dose taken within 72
hours of intercourse

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 INJECTABLE
• Developed to obviate need for daily ingestion of pills
• Given I.M. as oily solution, highly effective
• (1) Long acting progestin alone :-
• Injected once in 2-3 months depending on the steriod and
amount
Two compounds have been marketed :-
• (a) Depot medroxyprogesteron acetate (DMPA) 150 mg at 3
month intervals
• After i.m. injection peak blood level are reached in 3 weeks
and decline with a half life of 50 days
• (b) Norethindrone (Norethisteron) enanthate 200 mg at 2
month intervals
• (2) Long acting progestin + long acting estrogen once a month

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 SIDE EFFECTS OF ORAL
CONTRACEPTIVES
• Changes in:
– Weight
– Sexual desire
– Vaginal discharge
– Menstrual flow
– Breast size
– Blood pressure

• Other Common side effects:

– Breakthrough bleeding
– Nausea headaches
– Urinary tract infection
– Depression
– Gum inflammation
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 LIMITATION
• Animal data indicated carcinogenic potential but not
observed in human
• Risk of breast cancer (<35 year)
• Menstrual irregularities and amenorrhoea
• Return of fertility may take 6-30 months after dis-
continuation
• Weight gain & head ache occur in > 5% subject
• Bone mineral density may decrease in long term users
due to low estrogen level cause by Gn suppression

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 CIs
• Hypertension
• Diabetes
• MI
• Migraine
• Cancer
• Thromboembolism

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 Choice of OC
• First choice of an OC is a monophasic pill
containing 30 – 35 mcg of ethinyl estradiol
• POP less effective than COC and
associated with unpredictable menstrual
bleeding and increased frequency of
ovarian cysts
• POP must be taken at same time each
day to maintain contraceptive efficacy
• Multiphasic pills have lower hormone
dose per cycle
 Choice of OC
• Products containing 20 mcg of estradiol
may cause less bloating and breast
tenderness and preferred in women 40
years or older

• Increased risk of contraceptive failure

with missed doses.

• COC may improve acne symptoms

 Monitoring parameters
• Annual BP monitoring
• Blood glucose levels
• Annual cytologic screening for
cancer
• Monitor for weight gain,
headaches, acne and hair loss
Thank you

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